Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) wherein R1, R2, R3, R4 and R5 are as defined herein for Formula (IA), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Compounds which Modulate the CB2 Receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R¹, R², R³, R⁴, R⁵, and R⁶ are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof

A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5, and R6are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R 1 , R 2 , R 3 , R 4 , R 5 , and R 6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6, and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions and uses thereof

Compounds of Formula (IA), (IB), (IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of making them, pharmaceutical formulations, and uses thereof

A compound of Formula (I) wherein R1, R2, R3, R4, R5, and R6are as defined herein, or a tautomer, prodrug, solvate, or salt thereof, pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Compounds which modulate the CB2 receptor

Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula wherein, R1, R2, A, Y, X, Ar1 and Ar2 have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.

Compounds Which Modulate The CB2 Receptor

Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula wherein, R 1 , R 2 , A, Y, X, Ar 1 and Ar 2 have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.

Tec kinase inhibitors

Disclosed are compounds of formula(I): wherein Ar1, Ar2, R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.

GLUCOCORTICOID MIMETICS, METHODS OF MAKING THEM, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Therapeutic Uses of Compounds Which Selectively Modulate The CB2 Receptor

Compounds of formula (I) 43. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to one of - claims 1 , and one or more pharmaceutically acceptable carriers and/or adjuvants.53. A method of treating pain wherein the pain is chosen from acute pain claims 1 , visceral pain claims 1 , spasm of the gastrointestinal tract or uterus claims 1 , colics claims 1 , neuropathic pain claims 1 , inflammatory and nociceptive pain claims 1 , cancer pain and headache claims 1 , according to one of -.6. The method according to wherein neuropathic pain is chosen from low back pain claim 5 , non-herpetic neuralgia claim 5 , post herpetic neuralgia claim 5 , diabetic neuropathy claim 5 , nerve injury claim 5 , acquired immune deficiency syndrome (AIDS) related neuropathic pain claim 5 , head trauma related neuropathic pain claim 5 , painful traumatic mononeuropathy claim 5 , toxin and chemotherapy induced pain claim 5 , phantom limb pain claim 5 , painful polyneuropathy claim 5 , thalamic pain syndrome claim 5 , post-stroke pain claim 5 , central nervous system injury related neuropathic pain claim 5 , post surgical pain claim 5 , stump pain claim 5 , repetitive motion pain claim 5 , pain induced by post mastectomy syndrome related neuropathic pain claim 5 , multiple sclerosis related neuropathic pain claim 5 , root avulsions claim 5 , postthoracotomy syndrome related neuropathic pain claim 5 , neuropathic pain associated hyperalgesia and allodynia. This application is a continuation application of U.S. Ser. No. 12/564,132 filed Sep. 22, 2009 which claims benefit to U.S. provisional application Ser. No. 61/100,077 filed Sep. 25, 2008.1. Technical FieldThe present invention relates to novel compounds which modulate the CB2 receptor and their use as medicaments.2. Background InformationWO2008014199, WO2008039645 discuss the CB2 receptor, and the therapeutic uses of the CB2 receptor agonist compounds disclosed therein. It is believed that the ...

Sulfone Compounds Which Modulate The CB2 Receptor

Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Tetrazole Compounds Which Selectively Modulate The CB2 Receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Azetidine 2-Carboxamide Derivatives Which Modulate The CB2 Receptor

Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Pyrrolidine Compounds Which Modulate The CB2 Receptor

Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain. (I)

Oxadiazole inhibitors of leukotriene production

The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R 1 -R 5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes

OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compounds of formula (I) and (IA): 2. A compound according to claim 1 , wherein:{'sup': 1', '2, 'sub': '1-6', 'Rand Rtogether with the carbon atom to which they are attached is cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, 2.2.1 bicycloheptyl, oxetanyl, tetrahydrofuranyl, tetrahydropyranyl, pyrrolidinyl, piperidinyl, tetrahydrothienyl, wherein each carbocycle or heterocycle is optionally independently substituted with one to two groups selected from Calkyl and halogen;'}{'sup': 3', '3, 'sub': 1-3', '1-3', '1-3', '1-3', '1-3, 'Ris pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, pyrrolyl, imidazolyl, thienyl, furanyl or thiazolyl, wherein each Ris optionally independently substituted with one to three groups selected from Calkyl, Calkoxy, Calkylhydroxy, —CN, amino, Calkylamino and Cdialkylamino;'}{'sup': '4', 'Ris hydrogen, halogen or methyl;'}{'sup': 5', '6', '7', '8', '5', '9', '10', '11, 'Ris methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert. butyl, pentyl, hexyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl, cycloheptyl, cyclooctyl, phenyl, piperidinyl, piperazinyl, morpholinyl, thiomorpholinyl, pyrrolidinyl, tetrahydropyranyl, pyrrolyl, thienyl, furanyl, thiazolyl, oxazolyl, isoxazolyl, pyrazolyl, imidazolyl, triazolyl, dihydropyridinyl, pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl, quinolinyl, isoquinolinyl, indolyl, pyrrolopyridinyl, pyrrolopyrimidinyl, pyrazolopyrimidinyl, imidazopyridinyl, indazolyl, —C(O)—R, hydroxy or —NRR, wherein each Ris optionally independently substituted with one to three groups selected from R, Rand R;'}{'sup': 6', '9', '10', '11, 'sub': 1-3', '1-3, 'Ris azetidinyl, pyrrolidinyl, piperidinyl, piperazinyl, tetrahydropyranyl, morpholinyl, thiomorpholinyl, amino, Calkylamino, Cdialkylamino or —NH-5-6 membered heterocycle, each optionally independently substituted with one to three groups selected from R, Rand R;'}{'sup': 7', '8, 'sub': 1-5', 'n', '1-6, 'Rand Rare ...

Compounds Which Selectively Modulate The CB2 Receptor

Compounds of formula (I) 8. The compound according to and wherein{'sup': 1', '2, 'sub': '1-3', 'Rand Rtogether with the nitrogen atom to which they are attached form a ring chosen from morpholinyl, pyrrolidinyl and piperidinyl, each optionally substituted with 1 to 3 Calkyl.'}9. The compound according to claim 2 , and wherein{'sup': '2', 'sub': 1-3', '1-2, 'Ris cyclopropyl, cyclohexyl, tetrahydropyranyl, pyrrolidinyl or piperidinyl, each optionally independently substituted with 1 to 2 substituents chosen from Calkyl and Calkylsulfonyl.'}12. A compound of the formula (I) according to and wherein Rand Rcan cyclize to form a 4-6 membered heterocyclic ring.15. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to or and one or more pharmaceutically acceptable carriers and/or adjuvants.16. A method of treating pain comprising administering a therapeutically effective amount of a compound according to or .17. The method according to wherein the pain is chosen from acute pain claim 16 , visceral pain claim 16 , neuropathic pain claim 16 , inflammatory and nociceptive pain claim 16 , cancer pain and headache. 1. Technical FieldThe present invention relates to novel compounds which modulate the CB2 receptor and their use as medicaments.2. Background InformationWO2008014199, WO2008039645 discuss the CB2 receptor, and the therapeutic uses of the CB2 receptor agonist compounds disclosed therein. It is believed that the highly selective activation of the CB2 receptor with an agonist may offer avenues of harnessing the beneficial effects while avoiding the adverse effects seen with dual CB1/CB2 cannabinoid receptor agonists (see e.g. Expert Opinion on Investigational Drugs (2005), 14(6), 695-703). It is desirable therefore to provide agonists of CB2 with minimized CB1 activity.PCT Application Number PCT/US09/34464 discloses compounds having CB2 agonist activity. The compounds of the present invention differ structurally from the ...

HETEROCYCLIC COMPOUNDS AS INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compound of formula (I): 3. The compound according to claim 1 , wherein:A is carbon;or a pharmaceutically acceptable salt thereof.4. The compound according to claim 1 , wherein:A is nitrogen;or a pharmaceutically acceptable salt thereof.5. The compound according to claim 1 , wherein:{'sup': 1', '2', '1', '2, 'Rand Rare each independently hydrogen, methyl, ethyl, propyl, isopropyl, butyl, isobutyl, tert. butyl, pentyl, hexyl, with the proviso that both Rand Rare not simultaneously hydrogen;'}or a pharmaceutically acceptable salt thereof.6. The compound according to claim 1 , wherein:{'sup': 1', '2, 'Rand Rtogether with the carbon atom to which they are attached form a cyclopropyl, cyclobutyl, cyclopentyl, cylohexyl or tetrahydropyranyl ring;'}or a pharmaceutically acceptable salt thereof.7. The compound according to claim 1 , wherein:{'sup': 1', '2, 'sub': 1-4', '1-2', '3', '1-2, 'Rand Rare each independently Calkyl, hydroxy, Calkyl-O—CHor —O—Calkyl or a pharmaceutically acceptable salt thereof.'}8. The compound according to claim 1 , wherein:{'sup': '3', 'sub': 1-3', '1-3', '1-3', '1-3', '1-3, 'Ris pyridinyl, pyrimidinyl, pyrazinyl, pyridazinyl or pyrrolopyridinyl, wherein each heteroaryl ring is optionally independently substituted with one to three groups selected from Calkyl, —O—Calkyl, Calkylhydroxy, halogen, hydroxy, amino, Calkylamino and Cdialkylamino;'}or a pharmaceutically acceptable salt thereof.9. The compound according to claim 1 , wherein:{'sup': '4', 'Ris hydrogen or methyl;'}or a pharmaceutically acceptable salt thereof.10. The compound according to claim 1 , wherein:HET is a 5-11 membered heteroaryl group selected from indolyl, pyrrolopyridinyl, indazolyl, benzimidazolyl, benzoxazolyl, benzothiazolyl, imidazopyridinyl, quinolinyl and isoquinolinyl;or a pharmaceutically acceptable salt thereof.12. The compound according to claim 1 , wherein:{'sup': 5', '6', '7, 'claim-text': (a) —H,', '(b) —OH,', '(c) halogen,', '(d) — ...

BENZODIOXANE INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compounds of formula (I): 5. A pharmaceutical composition comprising one or more compounds of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , and a pharmaceutically acceptable carrier or excipient.6. A pharmaceutical composition comprising one or more compounds of claim 2 , or a pharmaceutically acceptable salt thereof claim 2 , and a pharmaceutically acceptable carrier or excipient.7. A pharmaceutical composition comprising one or more compounds of claim 3 , or a pharmaceutically acceptable salt thereof claim 3 , and a pharmaceutically acceptable carrier or excipient.8. A pharmaceutical composition comprising one or more compounds of claim 4 , or a pharmaceutically acceptable salt thereof claim 4 , and a pharmaceutically acceptable carrier or excipient.9. The pharmaceutical composition of claim 1 , further comprising at least one additional pharmacologically active substance.10. A method of treating leukotriene-mediated disorders comprising administering a pharmaceutically effective amount of a compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , to a patient in need thereof.11. The method of claim 10 , wherein the leukotriene-mediated disorder is a cardiovascular disease.12. A method of treating leukotriene-mediated disorders comprising administering the pharmaceutically composition of claim 5 , to a patient in need thereof.13. The method of claim 12 , wherein the leukotriene-mediated disorder is a cardiovascular disease. This invention relates to benzodioxanes that are useful as inhibitors of leukotriene Ahydrolase (LTAH) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of leukotrienes including asthma, allergy and cardiovascular diseases including atherosclerosis, myocardial infarction and stroke. This invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds ...

INHIBITORS OF LEUKOTRIENE PRODUCTION

The present invention relates to compounds of formula (I): 2. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein one of Aand Ais N and the other is CH.3. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ais N.4. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Aand Aare each CH.5. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Aand Aare each N.6. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein ring B is selected from the group consisting of B-1 claim 1 , B-2 claim 1 , B-3 claim 1 , B-4 claim 1 , B-5 and B-6.7. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris a group of formula —N(R)(R) claim 1 , wherein{'sup': 2', '3', '2', '3', '4, 'sub': 1', '6', '3', '6', '1', '6', '3', '6, 'Rand Rare each independently selected from the group consisting of —H, —(C-C)alkyl, —(C-C)cycloalkyl, and -(4- to 7-membered)heterocyclyl, wherein each of said —(C-C)alkyl, —(C-C)cycloalkyl, and -(4- to 7-membered)heterocyclyl of said Rand Rmay optionally be independently substituted by 1 to 3 Rgroups;'}{'sup': 4', '5', '5', '5', '5', '5, 'sub': 1', '6', '1', '6', '2', '2', '3', '6', '1', '6', '1', '6, 'Ris selected from the group consisting of halo, —OH, ═O, —(C-C)alkyl), —O(C-C)alkyl), —N(R), —C(O)—R, —N(R)—C(O)—R, —C(O)—N(R), —(C-C)cycloalkyl optionally substituted by —C(O)—(C-C)alkyl), -(4- to 7-membered)heterocyclyl optionally substituted by —C(O)—(C-C)alkyl), and phenyl; and'}{'sup': '5', 'sub': 1', '6', '3', '6, 'each Ris independently selected from the group consisting of —H, —(C-C)alkyl, —(C-C)cycloalkyl, and -(4- to 7-membered)heterocyclyl.'}8. The compound of claim 1 , or a pharmaceutically acceptable salt thereof claim 1 , wherein Ris selected from the group consisting of —N(H)((C-C)alkyl) claim 1 , —N((C-C)alkyl) claim 1 , —N(H)((4- ...

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I) 3. The compound according to and wherein{'sub': 2', '1-4, 'Cy is phenyl, pyridinyl, pyridazinyl, pyrimidinyl or pyrazinyl each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-3, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, R—S(O)—, —CN, —C(O)—NH(R) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '3', 'm, 'L is a linker chosen from a bond, O, >C(O), —CH—, —O—CH—, —NH—, —NH—CH—, —CH—NH—, —C(O)—NH—CH—, —NH—C(O)—NH— and —N(R)—S(O)—;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl, piperidinyl, piperazinyl or pyrrolidinylor a pharmaceutically acceptable salt thereof.4. The compound according to and wherein{'sub': 2', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-2, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, CH—S(O)—, —CN, —C(O)—NH(R) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '3', 'm, 'L is a linker chosen from a bond, O, >C(O), —CH—, —O—CH—, —NH—, —NH—CH—, —CH—NH—, —C(O)—NH—CH—, —NH—C(O)—NH— and —N(R)—S(O)—;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl or piperidinylor a pharmaceutically acceptable salt thereof.5. The compound according to and wherein{'sub': 2', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-2, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, CH—S(O)—, —CN, —C(O)—NH(CH) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '2, 'L is a ...

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I) 3. The compound according to and wherein{'sub': 2', '1-4, 'Cy is phenyl, pyridinyl, pyridazinyl, pyrimidinyl or pyrazinyl each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-3, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, R—S(O)—, —CN, —C(O)—NH(R) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '3', 'm, 'L is a linker chosen from a bond, O, >C(O), —CH—, —O—CH—, —NH—, —NH—CH—, —CH—NH—, —C(O)—NH—CH—, —NH—C(O)—NH— and —N(R)—S(O)—;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl, piperidinyl, piperazinyl or pyrrolidinylor a pharmaceutically acceptable salt thereof.4. The compound according to and wherein{'sub': 2', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-2, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, CH—S(O)—, —CN, —C(O)—NH(R) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '3', 'm, 'L is a linker chosen from a bond, O, >C(O), —CH—, —O—CH—, —NH—, —NH—CH—, —CH—NH—, —C(O)—NH—CH—, —NH—C(O)—NH— and —N(R)—S(O)—;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl or piperidinylor a pharmaceutically acceptable salt thereof.5. The compound according to and wherein{'sub': 2', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-2, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, CH—S(O)—, —CN, —C(O)—NH(CH) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '2, 'L is a ...

Heteroaromatic compounds as btk inhibitors

The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

Heteroaromatic compounds as btk inhibitors

The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I) 2. The compound according to wherein{'sub': 1', '1-4, 'Cy is phenyl, pyrazolyl, pyridinyl, pyrrolyl, imidazolyl, thiazolyl, furanyl, oxazolyl, isoxazolyl, thienyl, pyridazinyl, pyrimidinyl, pyrazinyl or pyranyl each is substituted by Rand optionally substituted by Calkyl, F, Cl or oxo;'}{'sub': '1', 'Ris chosen from{'sub': m', '3', '1', '1-4', '3', '2', '3', '1-3, 'L-Ar and —S(O)—R, each Ris optionally substituted by Br, Calkyl, R—S(O)—, —CN, —C(O)—NH(R) and Calkoxy;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl optionally substituted by benzyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl, piperidinyl, piperazinyl or pyrrolidinylor a pharmaceutically acceptable salt thereof.3. The compound according to wherein{'sub': 1', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl, oxo or Calkoxy;'}{'sub': 1', '1', '1-4', '3', '2', '3', '1-2, 'Ris L-Ar, each Ris optionally substituted by Br, Calkyl, CH—S(O)—, —CN, —C(O)—NH(R) and Calkoxy;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl optionally substituted by benzyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl or piperidinyl;or a pharmaceutically acceptable salt thereof.4. The compound according to wherein{'sub': 1', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl, oxo or Calkoxy;'}{'sub': 1-4', '3', '2', '3', '1-2, 'L-Ar is optionally substituted by F, Cl, Calkyl, CH—S(O)—, —CN, —C(O)—NH(CH) and Calkoxy;'}Ar is phenyl or pyrimidinyl;or a pharmaceutically acceptable salt thereof.10. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to or a pharmaceutically acceptable salt thereof.11. A method of treating a disease chosen from rheumatoid arthritis claim 1 , systemic lupus erythromatosis claim 1 , scleroderma claim 1 , asthma ...

HETEROAROMATIC COMPOUNDS AS BTK INHIBITORS

The present invention encompasses compounds of the formula (I) 3. The compound according to and wherein{'sub': 2', '1-4, 'Cy is phenyl, pyridinyl, pyridazinyl, pyrimidinyl or pyrazinyl each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-3, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, R—S(O)—, —CN, —C(O)—NH(R) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '3', 'm, 'L is a linker chosen from a bond, O, >C(O), —CH—, —O—CH—, —NH—, —NH—CH—, —CH—NH—, —C(O)—NH—CH—, —NH—C(O)—NH— and —N(R)—S(O)—;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl, piperidinyl, piperazinyl or pyrrolidinylor a pharmaceutically acceptable salt thereof.4. The compound according to and wherein{'sub': 2', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-2, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, CH—S(O)—, —CN, —C(O)—NH(R) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '3', 'm, 'L is a linker chosen from a bond, O, >C(O), —CH—, —O—CH—, —NH—, —NH—CH—, —CH—NH—, —C(O)—NH—CH—, —NH—C(O)—NH— and —N(R)—S(O)—;'}Ar is phenyl, pyridinyl, pyridazinyl, pyrimidinyl, pyrazinyl, benzoxazolyl, indolyl, isoindolyl, benzofuranyl, benzimidazolyl, benzothiazolyl or piperidinylor a pharmaceutically acceptable salt thereof.5. The compound according to and wherein{'sub': 2', '1-2, 'Cy is phenyl or pyridinyl, each is substituted by Rand optionally substituted by F, Cl or Calkoxy;'}{'sub': '2', 'Ris chosen from{'sub': 1-3', '1-3', '1-4', '3', '2', '3', '1-2, 'L-Ar and Calkoxy, each Ar and Calkoxy are optionally substituted by F, Cl, Calkyl, CH—S(O)—, —CN, —C(O)—NH(CH) or Calkoxy;'}{'sub': 2', '2', '2', '2', '2', '2, 'L is a ...

Compounds which modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the CB2 receptor

are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Tetrazole compounds which selectively modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Azetidine 2-carboxamide derivatives which modulate the CB2 receptor

Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Therapeutic uses of compounds which selectively modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Therapeutic uses of compounds which selectively modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Thiophene -2- carboxylic acid - (1h - benzimidazol - 2 yl) - amide derivatives and related compounds as inhibitors of the tec kinase itk (interleukin -2- inducible t cell kinase) for the treatment of inflammation, immunological and allergic disorders

Disclosed are compounds of formula (I): wherein Ar1, Ar2, R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.

1,1,1-trifluoro-4-phenyl-4-methyl-2-(1h-pyrrolo

Compounds of Formula (IA), IB), IC), and (ID) wherein R1, R2, R3, R4, R5, and R6 are as respectively defined herein for Formula (IA), (IB), (IC), and (ID), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Compounds which modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Tetrazole compounds which selectively modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Compounds which selectively modulate the cb2 receptor.

Se describen compuestos de fórmula (I)) (ver fórmula (I)) (ver fórmula (I)) Los compuestos de acuerdo con la invención se unen a y son agonistas, antagonistas o agonistas inversos del receptor CB2, y son útiles para tratar la inflamación. Los compuestos que son agonistas también son útiles para tratar el dolor.

Heteroaromatic compounds as BTK inhibitors

The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

Compounds which selectively modulate the CB2 receptor

Compounds which modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

1,2,1-Trifluoro-4-phenyl-4-methyl-2-(1H-pyrrolo[2,3-C]pyridin-2-ylmethyl)pentan-2-ol derivatives and related compounds as glucocorticoid ligands for the treatment of inflammatory diseases and diabetes.

Disclosed are compounds of Formula IA, IB, IC and ID wherein R1 is an optionally substituted aryl or heteroaryl group, R5 is an optionally substituted heteroaryl group and wherein the rest of the substituents are disclosed within the specification. Also disclosed is the preparation of a compound of formula IA, IB, IC or ID and the use of compound of formula IA, IB, IC and ID in the manufacture of a medicament for modulating glucocorticoid receptor function.

Sulfonyl compounds which selectively modulate the CB2 receptor

Compounds that modulate the CB2 receptor

Forbindelser med formel (I) er beskrevet. Forbindelser i henhold til oppfinnelsen binder til og er agonister, antagonister eller inverse agonister til CB2 reseptoren, og er nyttige for behandling av inflammasjon. De forbindelser som er agonister er i tillegg nyttige for behandling av smerte.

Heteroaromatic compounds as Bruton's tyrosine kinase (BTK) inhibitors

The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, XI and Y are defined herein, which are suitable for the treatment of a disease chosen from rheumatoid arthritis, systemic lupus erythromatosis, scleroderma, asthma, allergic rhinitis, allergic eczema, B cell lymphoma, multiple sclerosis, juvenile rheumatoid arthritis, juvenile idiopathic arthritis, inflammatory bowel disease, graft versus host disease, psoriatic arthritis, ankylosing spondylitis and uveitis.

Heteroaromatic compounds as BTK inhibitors

The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, X1 and Y are defined herein, which are suitable for the treatment of diseases related to BTK, process of making, pharmaceutical preparations which contain compounds and their methods of use.

Tetrazole compounds which selectively modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Oxadiazole inhibitors of leukotriene production

The present invention relates to compounds of formula (I) and (IA) and pharmaceutically acceptable salts thereof, wherein R 1 - R 5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Compounds selectively modulating the cb2 receptor

L'invention concerne des composés de formule (i), qui se lient au récepteur cb2 dont ils sont des agonistes, des antagonistes ou des agonistes inverses, et sont utiles pour le traitement d'une inflammation. Ceux des composés The invention relates to compounds of formula (i), which bind to the cb2 receptor of which they are agonists, antagonists or inverse agonists, and are useful for the treatment of inflammation. Those of compounds

Oxadiazole inhibitors of leukotriene production

The present invention relates to compounds of formula (I) and (IA) and pharmaceutically acceptable salts thereof, wherein R 1 - R 5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds of Formula (IA) and Formula (IB) wherein R1, R2, R3, R4, R5 and R6 are as defined herein for Formula (IA) or Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing su ch compounds, and methods of modulating the glucocorticoid receptor function an d methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Heterocyclic compounds which modulate the cb2 receptor

Oxadiazole inhibitors of leukotriene production.

La presente invención se refiere un compuesto de fórmula (I): (Ver Formula) o sales farmacéuticamente aceptables del mismo, en la que R1-R5 son como se definen en la presente memoria. La invención también se refiere a composiciones farmacéuticas que comprenden estos compuestos, a métodos para usar estos compuestos en el tratamiento de diversas enfermedades y trastornos, a procedimientos para preparar estos compuestos y a compuestos intermedios útiles en estos procedimientos.

Compounds which selectively modulate the CB2 receptor

Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them and uses thereof

A compound of Formula (I), wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

MIMETICS OF GLUCOCORTICOIDS, PROCEDURES FOR THE PREPARATION, PHARMACEUTICAL COMPOSITIONS AND THEIR USE OF THEM.

Compuestos de fórmula (IA) y fórmula (IB) en las que R1, R2, R3, R4, R5, y R6, son como se definen en la presente memoria para la fórnula (IA) o la fórmula (IB), o uno de sus tautómeros, profármacos, solvatos o sales, composiciones farmacéuticas que contienen dichos compuestos y procedimientos para modular la función del receptor de glucocorticoides y procedimientos para tratar estados de enfermedad o trastornos mediados por la función del receptor de glucocorticoides o caracterizados por procesos inflamatorios, alérgicos o proliferativos en un paciente usando estos compuestos. Compounds of formula (IA) and formula (IB) in which R1, R2, R3, R4, R5, and R6, are as defined herein for the formula (IA) or formula (IB), or one of its tautomers, prodrugs, solvates or salts, pharmaceutical compositions containing said compounds and procedures for modulating the function of the glucocorticoid receptor and procedures for treating disease states or disorders mediated by the function of the glucocorticoid receptor or characterized by inflammatory, allergic processes or proliferative in a patient using these compounds.

Sulfonyl compounds which selectively modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

GLUCOCORTICOID MIMETIC COMPOUNDS, METHODS OF PREPARATION AND PHARMACEUTICAL COMPOSITIONS

SE REFIERE A COMPUESTOS DE FORMULA (IB) DONDE R1 ES ARILO O HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS; R2 Y R3 SON CADA UNO ALQUILO C1-C5; R4 ES ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5 OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C3, HIDROXI, HALOGENO, AMINO, OXO; R5 ES HETEROARILO OPCIONALMENTE SUSTITUIDO CON ALCOXICARBONILO C1-C5, ALCANOILOXI C1-C5, AMINOCARBONILO, ENTRE OTROS; R6 ES H, ALQUILO C1-C8, ALQUENILO C2-C8, ENTRE OTROS, NO PUDIENDO SER TRIFLUOROMETILO, OPCIONALMENTE SUSTITUIDO CON ALQUILO C1-C5, ALQUENILO C2-C5, ALQUINILO C2-C5, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 2-CICLOPROPIL-4-(5-FLUORO-2-METOXIFENIL)-4-METIL-1-(1H-PIRROLO[3,2-c]PIRIDIN-2-IL)PENTAN-2-OL, METIL ESTER DEL ACIDO 4-(5-FLUORO-2-METOXIFENIL)-2-HIDROXI-4-METIL-2-(1H-PIRROLO[2,3-c]PIRIDIN-2-ILMETIL)PENTANOICO, 2-[2-DIFLUOROMETIL-2-HIDROXI-4-(5-METANSULFONIL-2,3-DIHIDROBENZOFURAN-7-IL)-4-METILPENTIL]-4-METIL-1H-INDOL-6-CARBONITRILO, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. DICHOS COMPUESTOS SON MODULADORES DEL RECEPTOR DE GLUCOCORTICOIDES SIENDO UTILES PARA EL TRATAMIENTO DE ENFERMEDADES PULMONARES, REUMATICAS, ALERGICAS, RENALES, HEPATICAS, CARDIOVASCULARES, NEUROLOGICAS, DIABETES TIPO I y II, OBESIDAD, ENFERMEDAD DE ALZHEIMER, ARTERIOESCLEROSIS, OSTEOARTRITIS, DOLOR GRAVE Y CRONICO REFERS TO FORMULA COMPOUNDS (IB) WHERE R1 IS ARYL OR HETEROARYL OPTIONALLY SUBSTITUTED WITH C1-C5 ALKYL, C2-C5 ALKENYL, C2-C5 ALKINYL, AMONG OTHERS; R2 AND R3 ARE EACH C1-C5 ALKYL; R4 IS C1-C5 ALKYL, C2-C5 ALKYL, C2-C5 ALKYL, OPTIONALLY SUBSTITUTED WITH C1-C3 ALKYL, HYDROXY, HALOGEN, AMINO, OXO; R5 IS HETEROARYL, OPTIONALLY SUBSTITUTED WITH C1-C5 ALCOXYCARBONYL, C1-C5 ALKANOYLOXY, AMINOCARBONYL, AMONG OTHERS; R6 IS H, C1-C8 ALKYL, C2-C8 ALKYL, AMONG OTHERS, IT CANNOT BE TRIFLUOROMETHYL, OPTIONALLY SUBSTITUTED WITH C1-C5 ALKYL, C2-C5 ALKENYL, C2-C5 ALKYL, AMONG OTHERS. PREFERRED COMPOUNDS ...

Glucocorticoid mimetics, pharmaceutical preparations and applications for the manufacture of drugs for the treatment of disease

Forbindelser med Formel (IA) og Formel (IB) hvor R, R, R, R, R5 og Rer som definert heri for Formel (IA) eller Formel (IB) eller en tautomer, prodrug, solvat eller salt derav; farmasøytiske preparater inneholdende slike forbindelser og metoder for å modulere glukocorticoidreseptorfunksjonen og metoder for behandling av sykdomstilstander eller forstyrrelser mediert av glukocorticoidreseptorfunksjonen ellerinflammatoriske, allergiske eller proliferative prosesser hos en pasient ved anvendelse av disse forbindelser.

Heteroaromatic compounds as bruton's tyrosine kinase (btk) inhibitors

The present invention encompasses compounds of the formula (I) wherein the groups A, Cy, XI and Y are defined herein, which are suitable for the treatment of a disease chosen from rheumatoid arthritis, systemic lupus erythromatosis, scleroderma, asthma, allergic rhinitis, allergic eczema, B cell lymphoma, multiple sclerosis, juvenile rheumatoid arthritis, juvenile idiopathic arthritis, inflammatory bowel disease, graft versus host disease, psoriatic arthritis, ankylosing spondylitis and uveitis.

Pyrrolidine compounds which modulate the cb2 receptor

compounds that selectively modulate the cb2 receptor

Compounds which selectively modulate the CB2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Arylsulfonamide compounds which modulate the cb2 receptor

Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) and the formula (IA) wherein, R1, R2, R3, R4, R5, R6, R7, R8 and X have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.

Compounds which modulate the cb2 receptor

Sulfonyl compounds which selectively modulate the CB2 receptor

Oxadiazole derived compounds, inhibitors of leukotriene production; pharmaceutical composition that includes it; and its use in the treatment of cardiovascular, inflammatory, allergic, pulmonary and fibrotic diseases and cancer.

Compuestos derivados bencil-oxadiazol, inhibidores de la producción de leucotrienos; composición farmacéutica; y su uso para trastornos como enfermedades cardiovasculares, inflamatorias, alérgicas, pulmonares y fibróticas, enfermedades renales y cáncer. Benzyl-oxadiazole derived compounds, inhibitors of leukotriene production; pharmaceutical composition; and its use for disorders such as cardiovascular, inflammatory, allergic, pulmonary and fibrotic diseases, kidney diseases and cancer.

Alpha-trifluoromethyl alcohols or amines as glucocorticoid mimetics

Compounds of Formula (I) wherein R1, R2, R3, R4, R5, R6 and X are as defined herein for Formula (IA) and Formula (IB), or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammtory, allergic, or proliferative processes in a patient using these compounds.

Glucocorticoid mimetics, methods of preparing them, pharmaceutical compositions and applications thereof

Forbindelser med Formel (IA) og Formel (IB) hvor R, R, R, R, Rog Rer ran definert heri for Formel (IA) eller Formel (IB) eller en tautomer, prodrug, solvit eller salt derav; farmasøytiske preparater inneholdende slike forbindelser og metoder for å modulere glukocorticoidieseptorfunksjonen og metoder forfnwg av sykdomstilstander eller forstyrrelser mediert av glukocoiticoidicseptoifunksjonen ellerinflammatoriske, allergiske eller proliferative prosesser hos en pasient ved anvendelse av disse forbindelser.

Compounds which selectively modulate the cb2 receptor

Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

1,1,1-Trifluoro-4-Phenyl-4-methyl-2-(1H-Pyrrolo

Heterocyclic Compounds Which Modulate The CB2 Receptor

Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Glucocorticoid mimetics, methods of making them, pharmaceutical formulations containing them, and uses thereof

A compound of Formula (I), wherein R1, R2, R3, R4, R5, and R6 are as defined herein, or a tautomer, prodrug, solvate, or salt thereof; pharmaceutical compositions containing such compounds, and methods of modulating the glucocorticoid receptor function and methods of treating disease-states or conditions mediated by the glucocorticoid receptor function or characterized by inflammatory, allergic, or proliferative processes in a patient using these compounds.

Oxadiazole inhibitors of leukotriene production

The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Sulfone compounds which modulate the cb2 receptor

Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.

Inhibitors of leukotriene production

本發明係關於式(I)之化合物：□或其醫藥上可接受的鹽，其中A1、A2、L1及B係如文中所定義。該等式(I)之化合物適用作白三烯A4水解酶(LTA4H)之抑制劑及治療與LTA4H相關的病變。本發明亦係關於包含式(I)之化合物之醫藥組合物、使用該等化合物於治療各種疾病及病變之方法及製備該等化合物之方法。

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Compounds which modulate the cb2 receptor

Compounds are provided which bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein, R1, R2, A, Y, X, Ar1 and Ar2 have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators.

1,1,1-trifluoro-4-phenyl-4-methyl-2-(1H-pyrrolo [2,3-C]pyridin-2-ylmethyl)pentan-2-ol Derivatives and related compounds as glucocorticoid ligands for the treatment of inflammatory diseases and diabetes.

Glucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

Oxadiazole inhibitors of leukotriene production

The present invention relates to compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R 1 -R 5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.

Glucocorticoid mimetika, verfahren zu ihrer herstellung, pharmazeutische formulierungen sie enthaltend und verwendungen davon

Clucocorticoid mimetics, methods of making them, pharmaceutical compositions, and uses thereof

COMPOUNDS OF FORMULA (IA) AND FORMULA (IB) WHEREIN R1,R2,R3,R4,R5, AND R6 ARE AS DEFINED HEREIN FOR FORMULA (IA) OR FORMULA (IB), OR A TAUTOMER, PRODRUG, SOLVATE, OR SALT THEREOF; PHARMACEUTICAL COMPOSITIONS CONTAINING SUCH COMPOUNDS, AND METHODS OF MODULATING THE GLOCOCORTICOID RECEPTOR FUNCTION AND METHODS OF TREATING DISEASE-STATES OR CONDITIONS MEDIATED BY THE GLUCOCORTICOID RECEPTOR FUNCTION OR CHARACTERIZED BY INFLAMMATORY, ALLERGIC, OR PROLIFERATIVE PROCESSES IN A PATIENT USING THESE COMPOUNDS.

Inhibitors of leukotriene production

The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein A 1 , A 2 , L 1 and B are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A 4 hydrolase (LTA 4 H) and treating LTA 4 H related disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.